EP1877091A4 - Verfahren zur verbesserung der pharmakokinetik von proteaseinhibitoren und proteaseinhibitorvorläufern - Google Patents
Verfahren zur verbesserung der pharmakokinetik von proteaseinhibitoren und proteaseinhibitorvorläufernInfo
- Publication number
- EP1877091A4 EP1877091A4 EP06741437A EP06741437A EP1877091A4 EP 1877091 A4 EP1877091 A4 EP 1877091A4 EP 06741437 A EP06741437 A EP 06741437A EP 06741437 A EP06741437 A EP 06741437A EP 1877091 A4 EP1877091 A4 EP 1877091A4
- Authority
- EP
- European Patent Office
- Prior art keywords
- protease
- improving pharmacokinetics
- inhibitor precursors
- protease inhibitor
- protease inhibitors
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/18—Sulfonamides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- AIDS & HIV (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US67508205P | 2005-04-27 | 2005-04-27 | |
PCT/CA2006/000685 WO2006114001A1 (en) | 2005-04-27 | 2006-04-26 | Method for improving pharmacokinetics of protease inhibitors and protease inhibitor precursors |
Publications (3)
Publication Number | Publication Date |
---|---|
EP1877091A1 EP1877091A1 (de) | 2008-01-16 |
EP1877091A4 true EP1877091A4 (de) | 2009-11-04 |
EP1877091B1 EP1877091B1 (de) | 2015-03-25 |
Family
ID=37214407
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP06741437.5A Active EP1877091B1 (de) | 2005-04-27 | 2006-04-26 | Verfahren zur verbesserung der pharmakokinetik von proteaseinhibitoren und proteaseinhibitorvorläufern |
Country Status (5)
Country | Link |
---|---|
US (2) | US20060287316A1 (de) |
EP (1) | EP1877091B1 (de) |
CA (1) | CA2606025A1 (de) |
ES (1) | ES2539527T3 (de) |
WO (1) | WO2006114001A1 (de) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7388008B2 (en) | 2004-08-02 | 2008-06-17 | Ambrilia Biopharma Inc. | Lysine based compounds |
CN101405293B (zh) * | 2005-11-30 | 2013-03-13 | 中裕新药股份有限公司 | 天冬氨酰基蛋白酶抑制剂基于赖氨酸的前体药物及其制备方法 |
JP2010502569A (ja) * | 2006-07-17 | 2010-01-28 | アンブリリア バイオファーマ インコーポレイテッド | 薬物動態学の改善方法 |
JP5401652B2 (ja) | 2006-09-21 | 2014-01-29 | タイメッド バイオロジクス インコーポレイテッド | プロテアーゼ阻害剤 |
WO2009148600A2 (en) * | 2008-06-06 | 2009-12-10 | Concert Pharmaceuticals, Inc. | Deuterated lysine-based compounds |
US8497383B2 (en) | 2009-05-27 | 2013-07-30 | Merck Sharp & Dohme Corp. | HIV protease inhibitors |
EP2632895B1 (de) | 2010-10-28 | 2018-10-03 | Merck Canada Inc. | Hiv-proteasehemmer |
US9187415B2 (en) | 2010-10-29 | 2015-11-17 | Merck Canada Inc. | Sulfonamides as HIV protease inhibitors |
WO2013059928A1 (en) | 2011-10-26 | 2013-05-02 | Merck Canada Inc. | Hiv protease inhibitors |
TWI678203B (zh) * | 2016-05-31 | 2019-12-01 | 中裕新藥股份有限公司 | 蛋白酶抑制劑之長效醫藥組合物 |
US10369129B2 (en) | 2016-05-31 | 2019-08-06 | Taimed Biologics, Inc. | Long acting pharmaceutical composition of protease inhibitor |
WO2017209732A1 (en) * | 2016-05-31 | 2017-12-07 | Taimed Biologics, Inc. | A long acting pharmaceutical composition of protease inhibitor |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6632816B1 (en) * | 2002-12-23 | 2003-10-14 | Pharmacor Inc. | Aromatic derivatives as HIV aspartyl protease inhibitors |
Family Cites Families (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5013861A (en) * | 1985-02-28 | 1991-05-07 | E. R. Squibb & Sons, Inc. | Ester substituted aminoalkanoylureido amino and imino acid and ester compounds |
US5614522A (en) * | 1990-11-19 | 1997-03-25 | G.D. Searle & Co. | Retroviral protease inhibitors |
JP4091653B2 (ja) * | 1992-08-25 | 2008-05-28 | ジー.ディー.サール、リミテッド、ライアビリティ、カンパニー | レトロウイルスプロテアーゼ阻害剤として有用なn−(アルカノイルアミノ−2−ヒドロキシプロピル)スルホンアミド |
JP4091654B2 (ja) * | 1992-08-25 | 2008-05-28 | ジー.ディー.サール、リミテッド、ライアビリティ、カンパニー | レトロウイルスプロテアーゼ阻害剤として有用なスルホニルアルカノイルアミノヒドロキシエチルアミノスルホンアミド |
US6022994A (en) * | 1992-08-25 | 2000-02-08 | G. D. Searle &. Co. | Succinoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors |
MX9603909A (es) * | 1994-03-07 | 1997-03-29 | Vertex Pharma | Derivados de sulfonamida como inhibidores de proteasa aspartilo. |
US5527829A (en) * | 1994-05-23 | 1996-06-18 | Agouron Pharmaceuticals, Inc. | HIV protease inhibitors |
US6143747A (en) * | 1995-01-20 | 2000-11-07 | G. D. Searle & Co. | Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors |
US5985870A (en) * | 1995-03-10 | 1999-11-16 | G.D. Searle & Co. | Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
US5776718A (en) * | 1995-03-24 | 1998-07-07 | Arris Pharmaceutical Corporation | Reversible protease inhibitors |
US6037157A (en) * | 1995-06-29 | 2000-03-14 | Abbott Laboratories | Method for improving pharmacokinetics |
PL328223A1 (en) * | 1996-01-26 | 1999-01-18 | Vertex Pharma | Aspartil protease inhibitors |
EP0877019B1 (de) * | 1997-05-09 | 2001-12-12 | Hoechst Aktiengesellschaft | Substituierte Diaminocarbonsäuren |
US6436989B1 (en) | 1997-12-24 | 2002-08-20 | Vertex Pharmaceuticals, Incorporated | Prodrugs of aspartyl protease inhibitors |
US6656985B1 (en) * | 1999-08-26 | 2003-12-02 | Dai Nippon Printing Co., Ltd. | Coloring material and color filter |
US6455587B1 (en) * | 2000-03-15 | 2002-09-24 | Pharmacor Inc. | Amino acid derivatives as HIV aspartyl protease inhibitors |
US6506786B2 (en) * | 2001-02-13 | 2003-01-14 | Pharmacor Inc. | HIV protease inhibitors based on amino acid derivatives |
CA2374362C (en) * | 2002-03-04 | 2008-01-22 | Brent Richard Stranix | Urea derivatives as hiv aspartyl protease inhibitors |
NZ541187A (en) * | 2002-12-16 | 2007-12-21 | Boehringer Ingelheim Int | Use of a combination containing a non-nucleoside reverse transcriptase inhibitor (NNRTI) with an inhibitor of cytochrome P450, such as protease inhibitors |
DE602004024584D1 (de) * | 2004-01-08 | 2010-01-21 | Medivir Ab | Inhibitoren der nicht-nukleotidischen reversen transkriptase |
US7388008B2 (en) * | 2004-08-02 | 2008-06-17 | Ambrilia Biopharma Inc. | Lysine based compounds |
-
2006
- 2006-04-26 EP EP06741437.5A patent/EP1877091B1/de active Active
- 2006-04-26 ES ES06741437.5T patent/ES2539527T3/es active Active
- 2006-04-26 CA CA002606025A patent/CA2606025A1/en not_active Abandoned
- 2006-04-26 US US11/380,291 patent/US20060287316A1/en not_active Abandoned
- 2006-04-26 WO PCT/CA2006/000685 patent/WO2006114001A1/en active Search and Examination
-
2011
- 2011-08-24 US US13/216,743 patent/US20120053139A1/en not_active Abandoned
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6632816B1 (en) * | 2002-12-23 | 2003-10-14 | Pharmacor Inc. | Aromatic derivatives as HIV aspartyl protease inhibitors |
Non-Patent Citations (5)
Title |
---|
KEAYS ET AL: "HIV infections", 20040201, vol. 5, no. 2, 1 February 2004 (2004-02-01), pages 54 - 57, XP005770445 * |
POIRIER J M ET AL: "Interet et limites du suivi therapeutique des inhibiteurs de la protease du VIH", REVUE FRANÇAISE DES LABORATOIRES, EDITIONS SCIENTIFIQUES ET MEDICALES ELSEVIER, vol. 2004, no. 365, 1 September 2004 (2004-09-01), pages 67 - 72, XP004825188, ISSN: 0338-9898 * |
See also references of WO2006114001A1 * |
STRANIX BRENT R ET AL: "Lysine sulfonamides as novel HIV-protease inhibitors: Nepsilon-disubstituted ureas", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 14, no. 15, 2 August 2004 (2004-08-02), pages 3971 - 3974, XP002544355, ISSN: 0960-894X * |
WAI LANG CHU: "HIV protease inhibitor impresses in preclinical trials", 18 October 2005 (2005-10-18), XP002544356, Retrieved from the Internet <URL:http://www.drugresearcher.com/content/view/print/24442> * |
Also Published As
Publication number | Publication date |
---|---|
ES2539527T3 (es) | 2015-07-01 |
US20120053139A1 (en) | 2012-03-01 |
EP1877091B1 (de) | 2015-03-25 |
EP1877091A1 (de) | 2008-01-16 |
WO2006114001A1 (en) | 2006-11-02 |
CA2606025A1 (en) | 2006-11-02 |
US20060287316A1 (en) | 2006-12-21 |
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Inventor name: WU, JINZI, J. Inventor name: MILOT, GUY Inventor name: GE, MICHAEL Inventor name: PETRELLA, MARCO Inventor name: STRANIX, BRENT, RICHARD Inventor name: PANCHAL, CHANDRA |
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